A general chemical principle for creating closure-stabilizing integrin inhibitors
<p>The paper establishes a chemical principle for designing integrin inhibitors that stabilize the inactive, closed conformation rather than the active, open conformation.</p>
<p>Integrins are proteins involved in cell adhesion and signaling. Many integrins exist in equilibrium between inactive closed and active open conformations. Small molecule integrin inhibitors can shift this equilibrium. Some stabilize the open state and are termed “opening” inhibitors. Others stabilize the closed state and are “closing” inhibitors.</p>
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